Abstract
We report herein the SAR studies of a series of indole- and indolizine-glyoxylamides that demonstrate substantial in vitro anti-proliferative activities against cancer cell lines, including multidrug resistance (MDR) phenotypes. The in vitro cytotoxic effects have been demonstrated across a wide array of tumor types of various origins (e.g., breast, colon, uterine).
MeSH terms
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ATP Binding Cassette Transporter, Subfamily B
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ATP Binding Cassette Transporter, Subfamily B, Member 1 / genetics
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ATP Binding Cassette Transporter, Subfamily B, Member 1 / metabolism
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Amides / chemical synthesis
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Amides / chemistry
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Amides / pharmacology*
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Antineoplastic Agents / chemical synthesis
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Antineoplastic Agents / chemistry
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Antineoplastic Agents / pharmacology*
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Blotting, Western
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Cell Death / drug effects
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Drug Resistance, Multiple*
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Fluorescent Antibody Technique
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Humans
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Indoles / chemistry*
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Indolizines / chemistry*
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Neoplasms / drug therapy*
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RNA, Messenger / genetics
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RNA, Messenger / metabolism
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Structure-Activity Relationship
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Tumor Cells, Cultured
Substances
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ABCB1 protein, human
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ATP Binding Cassette Transporter, Subfamily B
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ATP Binding Cassette Transporter, Subfamily B, Member 1
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Amides
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Antineoplastic Agents
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Indoles
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Indolizines
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RNA, Messenger
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indolizine
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indole